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Assay Detail

CHEMBL1953791

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human recombinant PDE4B2-mediated cAMP hydrolysis for 30 mins by colorimetric assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

3',5'-cyclic-AMP phosphodiesterase 4B (CHEMBL275)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dual β2-adrenoceptor agonists-PDE4 inhibitors for the treatment of asthma and COPD.
Shan WJ, Huang L, Zhou Q, Jiang HL, Luo ZH, Lai KF, Li XS.
Bioorg Med Chem Lett (2012) 22 : 1523 -1526
PubMed 22297114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.75 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL193240 ROFLUMILAST 4.0 1 9.00
CHEMBL511115 CILOMILAST 3.0 1 6.92
CHEMBL1951070 1 6.60
CHEMBL1951069 1 6.59
CHEMBL1951067 1 6.58
CHEMBL1951066 1 6.56
CHEMBL1951065 1 6.55
CHEMBL1951068 1 6.55
CHEMBL430893 (-)-ROLIPRAM 1 6.30
CHEMBL82318 1 6.28
CHEMBL124706 PHTHALAZINONE 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL193240 ROFLUMILAST IC50 = 1.0 nM 9.00
CHEMBL511115 CILOMILAST IC50 = 120.0 nM 6.92
CHEMBL1951070 IC50 = 251.0 nM 6.60
CHEMBL1951069 IC50 = 257.0 nM 6.59
CHEMBL1951067 IC50 = 265.0 nM 6.58
CHEMBL1951066 IC50 = 278.0 nM 6.56
CHEMBL1951065 IC50 = 280.0 nM 6.55
CHEMBL1951068 IC50 = 284.0 nM 6.55
CHEMBL430893 (-)-ROLIPRAM IC50 = 500.0 nM 6.30
CHEMBL82318 IC50 = 520.0 nM 6.28
CHEMBL124706 PHTHALAZINONE IC50 = 520.0 nM 6.28